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The following message was posted to: PharmPK
Dear all,
I am looking for drugs that bind significantly to lipoproteins. I was
able to find a few: probucol, cyclosporin, heparin, echinocandins. By
chance, do you have any further examples in mind? References would be
welcome. Many thanks in advance for your input.
Henri
Henri MERDJAN
Head of Drug Metabolism and Pharmacokinetics
NOVEXEL S.A., Parc Biocitech, 102 Route de Noisy
F-93230 Romainville, France
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The following message was posted to: PharmPK
Dear Henri
There is a communication about the binding of ivermectin and
moxidectin to lipoproteins.
This study was presented by A. Lespine on the 9th International
Congress of the European Association of Veterinary Pharmacology and
Toxicology.
Proceedings have been published on Journal of Veterinary
Pharmacology and Therapeutics (26) Suppl. 1, 2003 (abstract A-24,
in page 101)
Hope it helps
Fabiana
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Dear Henri,
Tacrolimus (FK506) is another example, some reports indicate that it
signifcantly binds to HDL:
[Zahir H, Nand RA, Brown KF, et al (2001)] Validation of methods to
study the distribution and protein binding of tacrolimus in human
blood. J.Pharmacol.Toxicol.Methods; 46 (1):27-35.
[Zahir H, McCaughan G, Gleeson M, et al (2004)] Factors affecting
variability in distribution of tacrolimus in liver transplant
recipients. Br.J.Clin.Pharmacol.; 57 (3):298-309.
[Nagase K, Iwasaki K, Nozaki K, et al (1994)] Distribution and
protein binding of FK506, a potent immunosuppressive macrolide
lactone, in human blood and its uptake by erythrocytes.
J.Pharm.Pharmacol.; 46 (2):113-7.
Regards,
Markus
Markus Weiss, PhD
ED/DMPK/ADME/ADE
Novartis Pharma AG, Werk Klybeck
WKL-135.4.83
CH-4002 Basel
Switzerland
Phone: +41 61 69 61075
Fax: +41 61 69 65146
Email : markus.weiss.-a-.novartis.com
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The following message was posted to: PharmPK
Dear Henri,
I recall another calcineurin inhibitor Tacrolimus (FK506) binds to
lipoproteins. Heres the reference.
1. Nagase, K., Iwasaki, K., Nozaki, K. & Noda, K. Distribution and
protein binding of FK506, a potent immunosuppressive macrolide lactone,
in human blood and its uptake by erythrocytes. J Pharm Pharmacol 46,
113-7. (1994).
Cheers
Alex
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The following message was posted to: PharmPK
Dear Henri
We have published about the binding of propofol to lipoproteins.
Zamacona MK, Suarez E, Garcia E, Aguirre C, Calvo R. Significance of
lipoproteins in serum binding variations of propofol. Anesth Analg
1998; 87: 1147-1151.
Leire de la Fuente, John C. Lukas, Nerea Jauregizar, Jose Antonio
Vazquez, Rosario Calvo, Elena Suarez."In vitro" binding of propofol to
serum lipoproteins in thyroid dysfunction. Eur J Clin Pharmacol
2002; 58: 615-619.
Hope it helps
Elena Suarez
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